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Assay Detail

CHEMBL820132

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro relative binding affinity for chick intestinal vitamin D3 receptor compared to [3H]1
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Gallus gallus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vitamin D3 receptor (CHEMBL2353)
Type SINGLE PROTEIN
Organism Gallus gallus

Publication

Synthesis of 1alpha,25-dihydroxyvitamin D3-26,23-lactams (DLAMs), a novel series of 1 alpha,25-dihydroxyvitamin D3 antagonist.
Kato Y, Nakano Y, Sano H, Tanatani A, Kobayashi H, Shimazawa R, Koshino H, Hashimoto Y, Nagasawa K.
Bioorg Med Chem Lett (2004) 14 : 2579 -2583
PubMed 15109656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.17 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431606 1 9.30
CHEMBL314009 1 8.72
CHEMBL315182 1 7.99
CHEMBL2114211 1 7.52
CHEMBL3350688 1 7.30
CHEMBL3350292 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431606 IC50 = 0.5 nM 9.30
CHEMBL314009 IC50 = 1.9 nM 8.72
CHEMBL315182 IC50 = 10.2 nM 7.99
CHEMBL2114211 IC50 = 30.0 nM 7.52
CHEMBL3350688 IC50 = 50.0 nM 7.30
CHEMBL3350292 IC50 > 100.0 nM -
CHEMBL3350292 IC50 > 100.0 nM -